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CAS No.: 879487-87-3

R-268712 Catalog No. CSN18520

Synonyms: R268712

R268712 is a potent and selective inhibitor of ALK5 with an IC50 of 2.5 nM.

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实验方案

技术信息

生物活性

描述The transforming growth factor β (TGF-β) is a key regulator of renal fibrosis that stimulates epithelial to mesenchymal transition and the production of extracellular matrix proteins. The activin receptor-like kinase 5 (ALK5) is a TGF-β type I receptor responsible for the phosphorylation of Smad 2/3 proteins. R268712 is a potent and selective ALK5 inhibitor with an IC50 value of 2.5 nM, but shows a weak inhibitory effect on p38 MAP kinase (IC50 = 12.1 μM). The administration of R268712 (1–10 mg/kg) in a mouse model of unilateral ureter obstruction inhibited renal luciferase activity in a dose-dependent manner. R268712 at a dosage of 1 mg/kg also significantly reduced proteinuria at day 21 post-treatment. In a heminephrectomized anti-Thy1 glomerulonephritis model, mice treated with R268712 at a concentration of 10 mg/kg showed suppressed weight gain compared with the control group^[2].
作用机制R268712 is a potent inhibitor of ALK5 that exhibits antifibrotic activity in a mouse model of unilateral ureter obstruction and a mouse model of anti-Thy1 glomerulonephritis^[2].
参考文献

[1] Terashima H, Kato M, et al. R-268712, an orally active transforming growth factor-β type I receptor inhibitor, prevents glomerular sclerosis in a Thy1 nephritis model. Eur J Pharmacol. 2014 Jul 5;734:60-6.
[2] Terashima H, Kato M, Ebisawa M, et al. R-268712, an orally active transforming growth factor-β type I receptor inhibitor, prevents glomerular sclerosis in a Thy1 nephritis model. Eur J Pharmacol. 2014;734:60‐66. doi:10.1016/j.ejphar.2014.03.045

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.7519 mL
- 13.7594 mL
- 27.5188 mL
- 5 mM
- 0.5504 mL
- 2.7519 mL
- 5.5038 mL
- 10 mM
- 0.2752 mL
- 1.3759 mL
- 2.7519 mL

技术信息

CAS号

879487-87-3

储存条件

粉末: Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C20H18FN5O

运输

蓝冰

分子量

363.39

别名

R268712

溶解度

DMSO	120.0 mg/mL (330.2 mM) warming

动物实验配方

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